Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1999-05-03
2000-06-06
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
A61K 3124
Patent
active
060719591
DESCRIPTION:
BRIEF SUMMARY
This invention relates to pharmaceutical products for the relief of pain, in particular the use of novel complexes of amide-type local anaesthetics, e.g. lignocaine, for treating pain and especially colic and other conditions of the lower gastrointestinal tract.
Numerous compounds have been examined in the last twenty years to find effective measures for the treatment of IBD. Such compounds include arsenicals, disodium cromoglycate, metronidazole, lignocaine, 4- and 5-aminosalicyclic acid as rectal preparations and orally administered thalidomide and cyclosporin. Rectal arsenic has been shown to be highly effective in ulcerative proctitis but is no longer widely used and, indeed, the therapeutic use of inorganic arsenical preparations is no longer recommended. The wide diversity of treatments is an indication of the complexity and intransigence of this condition.
The mainstay in drug therapy for ulcerative colitis has been corticosteroids and aminosalicylates but approximately one third of patients fail to go into complete remission despite this conventional therapy.
In spite of many attempts to provide an effective treatment for IBD, this chronic, distressing and ultimately life-threatening condition has not been well controlled.
Amide-type local anaesthetics have been used medically for many years. They produce a reversible loss of sensation by preventing or diminishing the conduction of sensory nerve impulses near to the site of their administration. They are most often used to ameliorate pain without loss of nervous control. Examples of amide-type local anaesthetics are aptocaine, bupivacaine, butanilicaine, carticaine, cinchocaine, clibucaine, ethyl parapiperidinoacetylaminobenzoate, etidocaine, lignocaine (also known as lidocaine), mepivacaine, oxethazaine, prilocaine, pyrrocaine, ropivacaine, tolycaine and vadocaine.
Amide-type local anaesthetics may be administered in a wide variety of different ways; some compounds are more suitable than others for a particular route of administration. For example, topical anaesthesia works by blocking the sensory nerve endings in the skin or mucous membranes. However, to reach these areas the compound must have good powers of penetration.
The amide-type local anaesthetics also vary in their anaesthetic potency, rate of onset and duration of effect. For example, lignocaine (2-diethylamino-N-[2,6-dimethylphenyl]acetamide) has a fast onset and an intermediate duration of action, and is employed in a wide range of anaesthetic applications. It is a white-yellow crystalline powder with a characteristic odour. It is practically insoluble in water.
Recently, it has been suggested (U.S. Pat. No. 5,331,013, The Lancet Journal, Jun. 11, 1988, p1330) to use a local anaesthetic such as lignocaine hydrochloride for treating ulcerative colitis and ulcerative proctitis. Arlander et al (Aliment. Pharmacol. Ther. 10, 73-81 (1996)) have also suggested that ropivacaine given rectally as a gel is effective in treating active distal ulcerative colitis.
There has been a need to improve the pharmacological effectiveness of amide-type local anaesthetics. The desired action of these anaesthetics is local, and absorption may lead to unwanted side-effects which may limit the duration, dosage or intensity of treatment.
We have found that lignocaine and other amide-type local anaesthetics are capable of forming a complex with polyacrylates and that the complexes are useful for relieving pain, particularly in the treatment of conditions of the gastrointestinal (GI) tract, e.g. irritable bowel syndrome and inflammatory bowel disorders such as Crohn's Disease and ulcerative colitis. Preferably the complex is a water-soluble complex.
One aspect of our invention provides a complex, preferably a water-soluble complex, of an amide-type local anaesthetic with a polyacrylate.
We surmise that the amide-type local anaesthetic complexes with the anionic carboxyl groups of the polyacrylate, modifies or enhances the therapeutic effect of the lignocaine. One way that it does this is to provide for a sustain
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Evans Brian Kenneth
Rhodes John
Rhodes Peter
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